Benzisoxazole spiropyrimidine triketone compounds and preparation method and use

A compound and mixture technology, applied in organic chemistry methods, organic chemistry, pharmaceutical formulations, etc., can solve problems such as limitations, unsatisfactory metabolic properties, and large clinical overdose, and achieve good druggability and excellent in vivo metabolic properties.
CN109111466BActive Publication Date: 2022-08-02SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
Publication Date
2022-08-02

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Abstract

The invention discloses a benzisoxazole spiropyrimidine trione compound, a preparation method and application thereof, and the structure is shown in formula I. In the formula, the definition of each substituent is as described in the specification and claims. The benzisoxazole spiropyrimidine trione compounds of the invention have higher antibacterial activity in vitro and in vivo and better metabolic properties.
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Description

technical field

[0001] The present invention relates to a spiropyrimidine trione compound containing benzisoxazole group, its pharmaceutical composition, its preparation method and use in anti-infective medicine. Background technique

[0002] With the widespread use and even abuse of antibacterial drugs, the multidrug resistance of pathogenic bacteria has become a serious problem that threatens human health. A series of drug-resistant pathogens represented by multidrug-resistant Staphylococcus aureus MRSA, It brings great challenges to clinical treatment. Although some new antibacterial drugs such as linezolid and daptomycin have been launched in recent years, which can effectively control the infection of gram-positive bacteria such as MRSA, but with more than 10 years of clinical application, bacteria have begun to slow down these drugs. Slowly producing resistant strains. Therefore, the development of novel antibacterial drugs with novel mechanism of action, unique stru...

Claims

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